Formulation and performance characterization of radio-sterilized "progestin-only" microparticles intended for contraception

AAPS PharmSciTech
Shivanand Puthli, Pradeep Vavia

Abstract

The aim of this study was to formulate and characterize a microparticulate system of progestin-only contraceptive. Another objective was to evaluate the effect of gamma radio-sterilization on in vitro and in vivo drug release characteristics. Levonorgestrel (LNG) microspheres were fabricated using poly(lactide-co-glycolide) (PLGA) by a novel solvent evaporation technique. The formulation was optimized for drug/polymer ratio, emulsifier concentration, and process variables like speed of agitation and evaporation method. The drug to polymer ratio of 1:5 gave the optimum encapsulation efficiency. Speed of agitation influenced the spherical shape of the microparticles, lower speeds yielding less spherical particles. The speed did not have a significant influence on the drug payloads. A combination of stabilizers viz. methyl cellulose and poly vinyl alcohol with in-water solvent evaporation technique yielded microparticles without any free drug crystals on the surface. This aspect significantly eliminated the in vitro dissolution "burst effect". The residual solvent content was well within the regulatory limits. The microparticles passed the test for sterility and absence of pyrogens. In vitro dissolution conducted on the product be...Continue Reading

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Citations

May 27, 2014·Materials Science & Engineering. C, Materials for Biological Applications·Martinha A AlmeidaPaulo V Farago
Mar 25, 2019·Pharmaceutics·Constantin MircioiuIon Mircioiu
Dec 29, 2020·Journal of Controlled Release : Official Journal of the Controlled Release Society·Sowmya Sivasankaran, Sriramakamal Jonnalagadda

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